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cyclooxygenase : ウィキペディア英語版 | cyclooxygenase
Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme () that is responsible for formation of prostanoids, including prostaglandins such as prostacyclin and thromboxane. The abbreviation "COX" is more often encountered in medicine. In genetics, the "PTGS" symbol is officially used for the prostaglandin-endoperoxide synthase (cyclooxygenase) family of genes and proteins, because the stem "COX" was already used for the cytochrome c oxidase family of genes and proteins. Pharmacological inhibition of ''COX'' can provide relief from the symptoms of inflammation and pain. Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The names "prostaglandin synthase (PHS)" and "prostaglandin endoperoxide synthetase (PES)" are still used to refer to COX. == Pharmacology ==
In terms of their molecular biology, ''COX-1'' and ''COX-2'' are of similar molecular weight, approximately 70 and 72 kDa, respectively, and having 65% amino acid sequence homology and near-identical catalytic sites. The most significant difference between the isoenzymes, which allows for selective inhibition, is the substitution of isoleucine at position 523 in ''COX-1'' with valine in ''COX-2''. The smaller Val523 residue in ''COX-2'' allows access to a hydrophobic side-pocket in the enzyme (which Ile523 sterically hinders). Drug molecules, such as DuP-697 and the coxibs derived from it, bind to this alternative site and are considered to be selective inhibitors of ''COX-2''.
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